Insulin Secretagogues

Question 1

Insulin Secretagogues cause what to occur?

Answer 1

Insulin to be secreted from beta cells in the pancreas

Question 2

Describe the regulation cascade for insulin to be secreted?

Answer 2

(+) Gs GPCR

• AC
• cAMP
• PKA
• Calcium current opened more to allow it in the cell
• Insulin leaves cell

Question 3

Which GPCR (-) the release of insulin by (-) the regulation cascade?

Answer 3

Gi

Question 4

What 2 things can (+) Gs GPCR to increase insulin secretion from the cell?

Answer 4

GLP-1 Agonists

Beta 2 Agonists

Question 5

What 2 things can (-) insulin secretion by (+) Gi GPCR?

Answer 5

Alpha 2 agonists

Somatostatin

Question 6

What are the 2 classes of Incretin Mimetics?

Answer 6

GLP-1 Agonists

DPP-4 Inhibitors

Question 7

What are the 2 GLP-1 Agonists?

Answer 7

Exenatide

Liraglutide

Question 8

What are the 2 GLP-1 Agonists?

Answer 8

Exenatide

Liraglutide

Question 9

What is the MOA for GLP-1 Agonists?

Answer 9

(+) Gs GPCR
- AC
- cAMP
- PKA
- Calcium influx
= Insulin release

Question 10

Which GLP-1 Agonist has the shorter half life?

Answer 10

Exenatide

Question 11

Which GLP-1 Agonist is bound to Albumin?

Answer 11

Liraglutide

Question 12

When are GLP-1 Agonists used?

Answer 12

Type 2 DM that is not well controlled when the patient is already on other meds

Question 13

Compared to other insulin secretagogues, how does the hypoglycemia risk compare with GLP-1 Agonists?

Answer 13

LOWER risk

Question 14

Normal Action of Incretins like GLP-1?

Answer 14

(+) insulin
(-) Glucagon
= Lower blood glucose postprandially

Question 15

How are GLP-1 Agonists and DPP-4 Inhibitors given?

Answer 15

GLP-1 Agonists = parenteral

DPP-4 Inhibitors = oral

Question 16

What is the normal job of DPP-4?

Answer 16

(-) GLP-1

= Increases blood glucose because insulin is not activated/glucagon not suppressed

Question 17

What are the DPP-4 Inhibitors?

Answer 17

• GLIPTINS

Question 18

What are the DPP-4 Inhibitors?

Answer 18

-GLIPTINS

Question 19

What 2 classes of drugs can block the K+ channel to increase insulin release?

Answer 19

Sulfonylureas

Meglitinides

Question 20

The 1st Gen Sulfonylureas are rarely used. What are they?

Answer 20

• AMIDES

Question 21

What are the 1st Gen Sulfonylureas?

Answer 21

• AMIDES

Question 22

Why are the 2nd Gen Sulfonylureas better?

Answer 22

Higher potency and LESS adverse effects

Question 23

What are the 2nd Gen Sulfonylureas?

Answer 23

GLI/Y ____

Question 24

What are the 2nd Gen Sulfonylureas?

Answer 24

GLY/I _____

Question 25

What is the MOA for the ____ AMIDES and GLY____? (sulfonylureas)

Answer 25

Block K+ channel

Question 26

What are 3 adverse effects of the Sulfonylureas?

Answer 26

Hypoglycemia
Weight gain
Secondary failure

Question 27

Sulfonylureas have many drug interactions. What happens if they are mixed with ethanol, CYP(-)s, NSAIDs?

Answer 27

INCREASE their hypoglycemic effect

Question 28

Sulfonylureas have many drug interactions. What happens if they are mixed with CYP(+)s, beta blockers or CCBs?

Answer 28

(-) glucose lowering effect

Question 29

What are the Meglitinides?

Answer 29

• GLINIDES

Question 30

What are the Meglitinides?

Answer 30

• GLINIDES

Question 31

When are - GLINIDES used?

Answer 31

Control postprandial hyperglycemia

Question 32

What are 3 adverse effects that can occur with - GLINIDEs?

Answer 32

Hypoglycemia
Weight gain
Secondary failure

Question 33

—— glinide

Answer 33

Meglitinides

= K+ channel blockers

Question 34

Gly/i —–

Answer 34

2nd Gen Sulfonylureas

= K+ channel blockers

Question 35

—– amide

Answer 35

1st Gen Sulfonylureas

= K+ channel blockers

Question 36

—- gliptins

Answer 36

DPP-4 Inhibitors

Question 37

Exenatide and Liraglutide are?

Answer 37

GLP-1 Agonists